Molecular Formula | C18H15N2NaO4 |
Molar Mass | 346.31247 |
Melting Point | >230°C (dec.) |
Solubility | DMSO (Slightly), Methanol (Slightly) |
Appearance | Solid |
Color | Yellow |
Storage Condition | Hygroscopic, -20°C Freezer, Under inert atmosphere |
In vitro study | Due to the allosteric mechanism, SSR128129E showed stronger activity in cell experiments. SSR128129E dose-dependently inhibited fgf2-induced EC proliferation and migration with IC50 of 31nM and 15.2nM, respectively. As a multitargeted FGFR inhibitor, SSR128129E inhibits FGFR1-4-mediated responses, resulting in blocked proliferation and/or migration in a variety of cell lines, such as mPanc02,HEK-hFGFR2WT,PAE-hFGFR1,hB9-myeloma and HUVEC. |
In vivo study | In arthritic mice, SSR128129E(30 mg/kg,p.o.) inhibited angiogenesis, inflammation, and bone resorption while relieving clinical symptoms. In various mouse tumor models, SSR128129E(30 mg/kg,p.o.) simultaneously inhibited primary tumor proliferation and metastasis. In addition, SSR128129E inhibited the proliferation of anti-vegfr2 recalcitrant tumor models and sensitive strains, while enhancing the anti-VEGFR2 antitumor activity. SSR128129E was also able to inhibit arteriosclerosis in intravenous grafts or in mouse models lacking apolipoprotein E. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.888 ml | 14.438 ml | 28.876 ml |
5 mM | 0.578 ml | 2.888 ml | 5.775 ml |
10 mM | 0.289 ml | 1.444 ml | 2.888 ml |
5 mM | 0.058 ml | 0.289 ml | 0.578 ml |